1. Metabolic Enzyme/Protease
    NF-κB
  2. MALT1
  3. MALT1 inhibitor MI-2

MALT1 inhibitor MI-2 

Cat. No.: HY-12276 Purity: 99.56%
Handling Instructions

MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to mice.

For research use only. We do not sell to patients.

MALT1 inhibitor MI-2 Chemical Structure

MALT1 inhibitor MI-2 Chemical Structure

CAS No. : 1047953-91-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 490 In-stock
Estimated Time of Arrival: December 31
100 mg USD 850 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

    MALT1 inhibitor MI-2 purchased from MCE. Usage Cited in: Parasit Vectors. 2018 May 18;11(1):305.

    The A20 protein levels in Jurkat T-cells and Molt-4 T-cells treated with MALT1 inhibitor MI-2 and combined use of MI-2 and ME-49.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to mice[1].

    IC50 & Target

    IC50: 5.84 μM (MALT1)[1]

    In Vitro

    MALT1 inhibitor MI-2 is a lead compound with nanomolar activity in cell-based assays and selective activity against ABC-DLBCLs. MI 2 is the most potent in cell-based assays, with 25% growth-inhibitory concentration (GI50) values in the high-nanomolar range. MI 2 induces significant selective dose-dependent suppression of ABC-DLBCL cells (p<0.0001). HBL-1 cells are treated with increasing concentrations of MI 2 for 24 hr and cleavage of the MALT1 target protein CYLD is measured by western blotting and densitometry. MI 2 causes a dose-dependent decrease in MALT1-mediated cleavage, noted by an increase in the uncleaved CYLD protein and a decrease in the cleaved form of the protein. MI 2 is selective as a MALT1 paracaspase inhibitor, because it displays little activity against the structurally related caspase family members caspase-3, -8, and -9. Moreover, MI 2 does not inhibit caspase-3/7 activity or apoptosis in cell-based assays at concentrations that suppress MALT1[1].

    In Vivo

    Five C57BL/6 mice were exposed to daily intraperitoneal (IP) administration of increasing doses of MALT1 inhibitor MI-2 ranging from 0.05 to 25 mg/kg over the course of 10 days to a cumulative dose of 51.1 mg/kg, and another five mice were exposed to vehicle only (5% DMSO, n=5). There is no evidence of lethargy, weight loss, or other physical indicators of sickness. To ascertain whether the maximal administered dose of 25 mg/kg is safe in a 14 day schedule, ten mice are exposed to daily IP administration of 25 mg/kg of MI 2 over 14 days to a cumulative dose of 350 mg/kg, using as controls five mice injected with vehicle only. Five mice are sacrificed after the 14 day course of MI 2 administration (together with the five controls) and the other five mice are sacrificed after a 10 day washout period to assess delayed toxicity. No toxic effects or other indicators of sickness, including weight loss or tissue damage (macroscopic or microscopic), are noted. Brain, heart, lung, liver, kidney, bowel, spleen, thymus, and bone marrow tissues are examined. Bone marrow is normocellular with trilineage maturing hematopoiesis. Myeloid-to-erythroid ratio is 4-5:1. Megakaryocytes are normal in number and distribution. There was no fibrosis or increased number of blasts or lymphocytes. Complete peripheral blood counts, biochemistry, and liver function tests are normal[1].

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 46 mg/mL (100.94 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1943 mL 10.9716 mL 21.9433 mL
    5 mM 0.4389 mL 2.1943 mL 4.3887 mL
    10 mM 0.2194 mL 1.0972 mL 2.1943 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [1]

    Cell number and viability are determined by trypan blue exclusion. Primary DLBCL cells are cultured in 96-well plates. Cells are grown in RPMI medium with 20% FBS supplemented with antibiotics for 48 hr. Cells are exposed to 0.8 µM MI 2 (1 µM for Pt.2) or control (DMSO) in quadruplicate. After 48 hr of exposure, viability is determined by using trypan blue. All samples are normalized to their own replicate control[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice[1]
    Eight-week-old male SCID NOD.CB17-Prkdcscid/J mice are subcutaneously injected with low-passage 107 human HBL-1, TMD8, or OCI-Ly1 cells in 50% Matrigel. Treatment is initiated when tumors reach an average size of 120 mm3. C57BL/6 mice are exposed to daily intraperitoneal (IP) administration of increasing doses of MI 2 ranging from 0.05 to 25 mg/kg over the course of 10 days to a cumulative dose of 51.1 mg/kg, and another five mice are exposed to vehicle only (5% DMSO, n=5). Tumor volume is monitored by digital calipering three times a week and calculated.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    455.72

    Formula

    C₁₉H₁₇Cl₃N₄O₃

    CAS No.

    1047953-91-2

    SMILES

    O=C(NC1=CC=C(N2N=C(OCCOC)N=C2C3=CC=C(Cl)C(Cl)=C3)C=C1)CCl

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.56%

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    Product Name:
    MALT1 inhibitor MI-2
    Cat. No.:
    HY-12276
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    MALT1 inhibitor MI-2

    Cat. No.: HY-12276